Computational approaches to aid PROTAC drug discovery

Sohini Chakraborti, Kirsten McAulay

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

Targeted protein degradation (TPD) has opened new avenues for targeting disease-causing proteins that were previously considered “undruggable.” PROTACs are among the most advanced TPD modalities and work by inducing proximity between a protein of interest (POI) and E3 ligase, facilitating degradation of the POI. The structural complexity of PROTACs means they generally fall beyond the Rule-of-five space and their rational design is highly challenging. In this chapter, we review state-of-the-art computational approaches for PROTAC design. We share our perspectives on how PROTAC designers can best leverage the available tools, despite known limitations, and discuss opportunities for future developments.
Original languageEnglish
Title of host publicationReference Module in Chemistry, Molecular Sciences and Chemical Engineering
PublisherElsevier
DOIs
Publication statusE-pub ahead of print - 21 Feb 2025

Publication series

NameReference Module in Chemistry, Molecular Sciences and Chemical Engineering
PublisherElsevier

Fingerprint

Dive into the research topics of 'Computational approaches to aid PROTAC drug discovery'. Together they form a unique fingerprint.

Cite this